Catalog No.
Product Name
Application
Product Information
Citations
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CDK inhibitor
NVP-LCQ195 is a small molecule heterocyclic inhibitor of CDK1, CDK2, CDK3 and CDK5 with IC50 of 1-42 nM. -
CDK inhibitor
Purvalanol A is a potent, cell-permeable cyclin-dependent protein kinase (cdk) inhibitor. IC50 values are 4, 70, 35, 850 and 75 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively. -
CDK8 inhibitor
CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor with an IC50 of 2.3 nM. -
CDK inhibitor
Voruciclib hydrochloride is a clinical stage orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. -
dual Cdc7/Cdk9 inhibitor
PHA-767491 hydrochloride is a dual Cdc7/Cdk9 inhibitor, with IC50s of 10 nM and 34 nM, respectively. -
CDK9 inhibitor
CDKI-73 is a potent CDK9 inhibitor with Ki of 4 nM; shows selective toxicity to CLL cells(LD50=80 nM) versus normal B cell and normal CD34+ cell(LD50>20 uM). -
CDK8 inhibitor
SEL120-34A HCl is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity. -
CDK1 Inhibitor
Avotaciclib is an orally active inhibitor of cyclin-dependent kinase 1 (CDK1). It effectively inhibits tumor cell proliferation and induces apoptosis, making it a valuable compound for cancer research. This reagent is particularly relevant in the study of cancers, including pancreatic and lung cancer, where CDK1 plays a critical role in cell cycle regulation and tumor growth. -
Cyclins/Cdk Inhibitor
Aminopurvalanol A is a selective inhibitor of Cyclins/Cdk complexes, primarily targeting the G2/M-phase transition. This compound effectively inhibits cancer cell differentiation and proliferation, making it a valuable tool for cancer research. Additionally, Aminopurvalanol A has been shown to disrupt sperm fertilizing ability by inhibiting capacitation-dependent actin polymerization, highlighting its potential in reproductive biology studies. -
CDK9 Inhibitor
(-)-Enitociclib is a selective inhibitor of cyclin-dependent kinase 9 (CDK9), with demonstrated capacity to induce apoptosis in various cancer cell lines. By inhibiting CDK9, it effectively reduces phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase II, leading to downregulation of critical oncogenes such as MYC and MCL1. This compound exhibits significant anti-proliferative effects against MYC-positive lymphoma and multiple myeloma cells, and shows synergistic potential when combined with therapies such as Bortezomib and Lenalidomide, making it a valuable tool in hematological cancer research. -
CDK4/6 PROTAC Degrader
PROTAC CDK4/6 degrader 1 is a dual-targeted degrader designed to selectively degrade cyclin-dependent kinases CDK4 and CDK6. With DC50 values of 10.5 nM and 2.5 nM, this compound effectively inhibits cell proliferation in Jurkat cells, demonstrating an IC50 of 0.18 μM. The compound promotes G1 phase cell cycle arrest and triggers apoptosis, making it a valuable tool for studying cancer biology and potential therapeutic applications in CDK-related malignancies. -
CDK12/CCNK Molecular Glue
NCT02 is a molecular glue degrader that targets CDK12 through the E3 ubiquitin ligase DDB1, resulting in the ubiquitination and subsequent proteasomal degradation of its partner protein CCNK. This mechanism leads to the downregulation of CDK12, inhibiting its downstream signaling pathways. NCT02 exhibits significant biological activity by inducing apoptosis in tumor cells, arresting the cell cycle, and selectively inhibiting the proliferation of colorectal cancer cells with TP53 mutations or belonging to the CMS4 molecular subtype. Additionally, NCT02 demonstrates potential in suppressing tumor growth in both in vitro and in vivo models. -
CDK8 Inhibitor
CDK8-IN-13 is a potent and selective inhibitor of cyclin-dependent kinase 8 (CDK8), exhibiting an IC50 value of 51.9 nM. This compound induces apoptosis and modulates the expression of phosphorylated STAT1 at serine 727 and STAT5 at serine 726. Due to its antitumor properties, CDK8-IN-13 is valuable for research applications focusing on cancer biology and therapeutic development targeting the CDK8 pathway. -
CCND1/CDK4 PROTAC Degrader
CPD-10 is a targeted CCND1 and CDK4 PROTAC degrader that effectively promotes the degradation of these proteins. Exhibiting significant anti-proliferative activity, CPD-10 induces apoptosis in cancer cell lines. It decreases the expression levels of cyclin D1, cyclin D3, CDK4, and phosphorylated Rb at serines 5807 and 811 in a dose-dependent manner, making it a valuable tool for research in cancer biology and therapeutic applications targeting cell cycle regulation. -
CDK7 Inhibitor
Samuraciclib is a selective, ATP-competitive inhibitor of CDK7, exhibiting an IC50 of 41 nM. This compound demonstrates significant selectivity over CDK1, CDK2, CDK5, and CDK9, with fold selectivities of 45, 15, 230, and 30, respectively. Samuraciclib effectively inhibits the proliferation of breast cancer cell lines, with GI50 values ranging from 0.2 to 0.3 μM, indicating its potential as an effective therapeutic agent in oncology research. -
CDK1 Inhibitor
Avotaciclib trihydrochloride is an orally active inhibitor of cyclin-dependent kinase 1 (CDK1). This compound has demonstrated the ability to inhibit tumor cell proliferation and induce apoptosis, making it a valuable tool for cancer research. Avotaciclib trihydrochloride is particularly relevant for studies focused on pancreatic and lung cancers. -
CDK4 Inhibitor
CDK4-IN-3 is a potent irreversible inhibitor of cyclin-dependent kinase 4 (CDK4), exhibiting an IC50 of 25 nM and demonstrating over 10-fold selectivity for CDK4 compared to CDK6. This compound effectively arrests the cell cycle in the G₁ phase, leading to the induction of apoptosis in tumor cells. CDK4-IN-3 is valuable for research applications focused on solid tumors, including breast and lung cancers. -
CDK1 Inhibitor
CGP-74514 is a potent and selective inhibitor of cyclin-dependent kinase 1 (CDK1), exhibiting an IC50 of 25 nM. By targeting the CDK1/cyclin B complex, CGP-74514 effectively halts the cell cycle at the G2/M phase and triggers apoptosis in tumor cells. This compound is particularly valuable for research focused on bladder cancer and related therapeutic applications. -
PROTAC CDK4/6 degrader
HEMTAC CDK4/6 degrader 1 is a PROTAC designed to target CDK4 and CDK6 through a dual-ligand approach involving HSP90. This compound effectively induces the degradation of CDK4/6 in B16F10 melanoma cells, leading to cell cycle arrest at the G0/G1 phase and subsequent apoptosis. It serves as a vital tool for cancer research, particularly in elucidating mechanisms of CDK4/6 regulation and their role in tumor progression. Additionally, HEMTAC CDK4/6 degrader 1 features an alkyne functional group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing compounds for advanced applications in chemical biology. -
CDK Inhibitor
CDK9-IN-7 is a selective and potent inhibitor of cyclin-dependent kinase 9 (CDK9), demonstrating an IC50 of 11 nM. This compound selectively inhibits CDK9 over other cyclin-dependent kinases, such as CDK4 and CDK6, with IC50 values of 148 nM and 145 nM, respectively. CDK9-IN-7 exhibits significant antitumor activity, inducing apoptosis in non-small cell lung cancer (NSCLC) cells, arresting the cell cycle in the G2 phase, and reducing the stemness characteristics of NSCLC. It is a valuable tool for research into cancer biology and potential therapeutic applications. -
Pan-CDK Inhibitor
AG-012986 is a potent pan-CDK inhibitor targeting multiple cyclin-dependent kinases including CDK1, CDK2, CDK4, CDK5, CDK6, and CDK9. It demonstrates significant biological activity with Kis of 9.2 nM for CDK4/cyclin, 44 nM for CDK1/cyclin B, and 94 nM for CDK2/cyclin A, alongside IC50 values of 4 nM for CDK9/cyclin T and 22 nM for CDK5/p35. AG-012986 effectively inhibits cell proliferation in cancer cell lines, inducing cell cycle arrest and apoptosis, making it a valuable tool for cancer research and therapeutic development. -
CDK2/JAK2/FLT3 Inhibitor
(E/Z)-Zotiraciclib hydrochloride is a potent inhibitor of CDK2, JAK2, and FLT3, exhibiting IC50 values of 13 nM, 73 nM, and 56 nM, respectively. This orally active compound demonstrates significant efficacy in inhibiting the proliferation of various cancer cell lines. It is a valuable tool for research into therapeutic strategies targeting cell cycle regulation and signal transduction pathways in cancer. -
CDK Inhibitor
RGB-286638 free base is a potent CDK inhibitor targeting cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5, with IC50 values of 1, 2, 3, 4, 5, and 5 nM, respectively. Additionally, it inhibits GSK-3β, TAK1, Jak2, and MEK1, exhibiting IC50 values of 3, 5, 50, and 54 nM. This compound is valuable for research in cell cycle regulation, cancer therapeutics, and signaling pathways involving kinase activity. -
CDK2/JAK2/FLT3 Inhibitor
(E/Z)-Zotiraciclib citrate is a potent inhibitor targeting CDK2, JAK2, and FLT3 kinases. This compound demonstrates significant biological activity in disrupting cell cycle progression and signaling pathways associated with cell proliferation and survival. It is utilized in cancer research applications, particularly for studies involving hematological malignancies and solid tumors where these kinases are dysregulated. -
CDK2/JAK2/FLT3 Inhibitor
Zotiraciclib hydrochloride is a novel small molecule inhibitor targeting cyclin-dependent kinase 2 (CDK2), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase 3 (FLT3). This reagent demonstrates anti-tumor activity by downregulating the Myc oncogene through CDK9 inhibition, contributing to reduced tumor growth. Zotiraciclib hydrochloride is particularly relevant for research into cancers capable of crossing the blood-brain barrier, and elevated levels of the MCL-1 protein may indicate its potential as a prognostic marker and therapeutic target in cancer studies. -
CDK Inhibitor
3-Methylthienyl-carbonyl-JNJ-7706621 is a selective cyclin-dependent kinase (CDK) inhibitor, demonstrating potent activity with IC50 values of 6.4 nM for CDK1/cyclin B and 2 nM for CDK2/cyclin A. Additionally, it exhibits strong inhibition of GSK-3 (IC50=0.041 μM) and moderate inhibition against CDK4, VEGF-R2, and FGF-R2 with IC50s of 0.11, 0.13, and 0.22 μM, respectively. This compound is primarily utilized in cancer research to explore CDK-related pathways and therapeutic strategies. -
CDK Inhibitor
DCB-3503 is an allosteric modulator targeting heat shock cognate protein HSC70, functioning as an inhibitor of Cyclin D1. By allosterically modulating the ATPase and chaperone activities of HSC70, DCB-3503 effectively inhibits the translation of Cyclin D1. This compound holds potential for research applications focused on malignancies characterized by elevated Cyclin D1 expression, such as hepatocellular carcinoma and breast cancer. -
CDK7 Inhibitor
Q901 is a potent and selective CDK7 inhibitor, exhibiting an IC50 of 10 nM. It effectively disrupts the activity of MYC and E2F, making it a valuable tool for studying cellular mechanisms in various cancer types, including colon and lung cancer. This compound is suitable for research applications focused on cancer biology and therapeutic development targeting CDK7. -
CDK9 Inhibitor
FIT-039 is a selective CDK9 inhibitor that acts as an ATP-competitive antagonist, exhibiting an IC50 of 5.8 μM against the CDK9/cyclin T1 complex. This compound demonstrates potent antiviral activity, effectively inhibiting the replication of various viruses, including HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human cytomegalovirus (CMV). FIT-039 is particularly notable for its potential in addressing drug-resistant strains of HSV and other DNA viruses in research applications. -
CK1/CDK1/CDK5 Inhibitor
(R)-DRF053 dihydrochloride is a selective inhibitor of casein kinases 1 (CK1), CDK1/cyclin B, and CDK5/p25, exhibiting IC50 values of 14 nM, 220 nM, and 80 nM, respectively. This compound effectively inhibits the CK1-mediated generation of amyloid-beta in cellular models, making it valuable for research into neurodegenerative diseases and cellular signaling pathways. Its specificity and potency position it as a suitable reagent for investigating the roles of these kinases in various biological processes. -
CDK8 Inhibitor
P162-0948 is a selective inhibitor of Cyclin-Dependent Kinase 8 (CDK8), demonstrating an IC50 value of 50.4 nM. This compound effectively reduces cell migration and downregulates the expression of epithelial-mesenchymal transition (EMT)-related proteins in A549 human alveolar epithelial cells. Additionally, P162-0948 inhibits Smad phosphorylation, indicating its potential to disrupt the TGF-β/Smad signaling pathway. This makes P162-0948 a valuable tool for research focused on pulmonary fibrosis and related pathways. -
CDK8 Inhibitor
CDK8-IN-11 is a potent and selective inhibitor of cyclin-dependent kinase 8 (CDK8), displaying an IC50 value of 46 nM. This compound effectively inhibits the WNT/β-catenin signaling pathway, making it a valuable tool for investigating the molecular mechanisms underlying oncogenesis. CDK8-IN-11 is primarily utilized in research related to colon cancer, contributing to the development of targeted therapeutic strategies. -
CDK6/9 Inhibitor
CDK6/9-IN-2 is a potent dual inhibitor of cyclin-dependent kinases CDK6 and CDK9, with reported IC50 values of 15 nM and 22 nM, respectively. This compound exhibits selectivity for CDK2, CDK8, and CDK11. CDK6/9-IN-2 effectively inhibits the proliferation of HaCaT cells stimulated by IFN-γ and TNF-α, while also suppressing the STAT3 signaling pathway and the expression of inflammatory factors. Its ability to alleviate psoriatic dermatitis makes CDK6/9-IN-2 valuable for research in psoriasis and related inflammatory conditions. -
CDK Inhibitor
AS2863619 free base is a selective inhibitor of cyclin-dependent kinases 8 and 19 (CDK8 and CDK19), demonstrating IC50 values of 0.61 nM and 4.28 nM, respectively. This compound drives the conversion of antigen-specific effector and memory T cells into Foxp3+ regulatory T (Treg) cells, thereby offering potential therapeutic approaches for various immunological conditions. The inhibition of CDK8/19 by AS2863619 enhances STAT5 activation, leading to the upregulation of the Foxp3 gene and promoting Treg cell development. -
CDK3 Inhibitor
Vanicoside B is a potent inhibitor of cyclin-dependent kinase 8 (CDK8), derived from the herb Persicaria dissitiflora. This compound demonstrates significant anti-tumor activity by disrupting CDK8-mediated signaling pathways and reducing the levels of proteins associated with epithelial-mesenchymal transition. As a result, Vanicoside B induces cell cycle arrest and apoptosis, making it a valuable reagent for cancer research and therapeutic investigations targeting CDK8 pathways. -
CDK8/19 Inhibitor
CDK8/19-IN-2 is a potent and orally active inhibitor of cyclin-dependent kinases 8 and 19, exhibiting IC50 values of 2.08 nM and 2.49 nM, respectively. This compound is crucial for research focusing on acute myeloid leukemia (AML), breast cancer, and lymphoma, where inhibition of CDK8 and CDK19 can influence tumor proliferation and survival. Its selectivity and efficacy make it a valuable tool in studying the role of these kinases in various oncogenic pathways. -
CDK8/19 Inhibitor
CDK8-IN-16 is a potent dual inhibitor of cyclin-dependent kinases 8 and 19, demonstrating IC50 values of 5.1 nM and 5.6 nM, respectively. This compound effectively inhibits phospho-STAT1SER727 with an IC50 of 17.9 nM in SW620 cells and modulates the WNT signaling pathway with an IC50 of 7.2 nM in 7dF3 cells. CDK8-IN-16 exhibits favorable pharmacokinetic properties, including an oral bioavailability of 57% in rat models, making it a valuable tool for research in cancer biology and therapeutic development. -
CDK9/FLT3 Inhibitor
CDDD11-8 is a potent and selective inhibitor of cyclin-dependent kinase 9 (CDK9) and FLT3-ITD, exhibiting Ki values of 8 nM and 13 nM, respectively. This compound effectively reduces the proliferation of leukemia cell lines, particularly those associated with the FLT3-ITD mutation. CDDD11-8 serves as a valuable tool for research into targeted therapies for hematological malignancies, specifically in the study of cell cycle regulation and tyrosine kinase signaling pathways. -
FLT3/CDK5 Inhibitor
AMG 925 (HCl) is a potent dual inhibitor targeting FLT3 and CDK5, demonstrating IC50 values of 2±1 nM and 3±1 nM, respectively. This compound exhibits selectivity for these kinases, making it a valuable tool for research into hematological malignancies and cancer progression. Its oral bioavailability further enhances its utility in preclinical studies investigating therapeutic interventions for FLT3-driven malignancies and CDK5-associated diseases. -
FLT3/CDK4 Inhibitor
FLT3/CDK4-IN-1 is a highly selective, orally active dual inhibitor targeting FLT3 and CDK4, demonstrating IC50 values of 11 nM and 7 nM, respectively. This compound exhibits significant antiproliferative activity against specific cancer cell lines and shows promising antitumor effects in vivo. FLT3/CDK4-IN-1 is suitable for research applications focused on cancer biology, particularly in exploring pathways associated with leukemias and solid tumors. -
CDK Inhibitor
(E/Z)-SU9516 is a selective inhibitor of cyclin-dependent kinases (CDKs), primarily targeting CDK2, with an IC50 value of 22 nM. This compound also exhibits inhibitory effects on CDK1 and CDK4, with IC50 values of 40 nM and 200 nM, respectively. Its potent inhibition of CDKs makes (E/Z)-SU9516 a valuable tool for studying cell cycle regulation and therapeutic applications in cancer research. -
CDK4 Inhibitor
3-ATA is a selective inhibitor of cyclin-dependent kinase 4 (CDK4), demonstrating both neuroprotective and antitumor properties. This compound has been shown to reduce kainic acid-induced apoptosis in cerebellar granule neurons, making it a valuable tool for investigating neurodegenerative diseases. Its ability to modulate cell cycle progression and prevent neuronal death highlights its potential applications in both cancer research and neuroprotection studies. -
CDK9-Cyclin T1 PPI Inhibitor
CDK9-Cyclin T1 PPI-IN-1 is a selective inhibitor of the CDK9-Cyclin T1 protein-protein interaction. This compound effectively inhibits cell proliferation in triple-negative breast cancer (TNBC) MDA-MB-231 cells with an IC50 of 0.044 μM and promotes apoptosis. Additionally, CDK9-Cyclin T1 PPI-IN-1 suppresses CDK9 transcriptional activity and diminishes the phosphorylation of RNA Polymerase II at the CTD serine 2 residue. In vivo studies further demonstrate its capability to inhibit tumor growth in a TNBC 4T1 mouse model.
